Method for reducing inflammation and inducing an analgesic...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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C514S557000, C514S578000, C514S825000, C514S886000, C514S019300

Reexamination Certificate

active

06495514

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The invention relates to a method for reducing inflammation and a method for inducing an analgesic effect in a subject and compounds thereof
2. Background Art
Inflammatory disease represents a pressing public health problem in our society. While rheumatoid arthritis is probably the most widely known chronic inflammatory disease, other examples are ulcerative colitis, Crohn's disease, gout, bursitis and tendinitis. Traditionally, inflammation has been treated with aspirin-like drugs, steroid based compounds, or non-steroidal anti-inflammatory drugs. These drugs are of variable effectiveness; however, they are not therapeutic in nature.
Neuropeptides are released from peripheral terminals of primary afferent sensory nerves and contribute significantly to the inflammatory response of a variety of diseases including rheumatoid arthritis. Examples of neuropeptides that have been investigated extensively are substance P (SP) and Calcitonin Gene-Related Peptide (CGRP). These neuropeptides have been shown to be capable of producing vasodilation, increasing vascular permeability, attracting and activating phagocytic white blood cells, releasing cytokines, lysosomal enzymes and prostaglandins from these cells, increasing the expression of adhesion molecules as well as causing the activation of synoviocytes.
Several pharmacological approaches to reduce the neurogenic component of inflammation have been evaluated; however, a means for reducing inflammation by reducing the release of a. neuropeptide responsible for inflammation has not been developed.
Thus, there remains a need in the art for reducing inflammation in a subject. Applicants have discovered such a method, and have also discovered a method for inducing an analgesic effect in a subject. The prior art does not disclose the methods or compounds such as those described and claimed herein.
SUMMARY OF THE INVENTION
In accordance with the purpose(s) of this invention, as embodied and broadly described herein, this invention, in one aspect, relates to a method for reducing inflammation in a subject, comprising administering to the subject an effective amount of the compound having the structure I or II:
wherein,
R
1
is C
1
-C
10
branched or straight chain alkyl, aryl, an amino acid, or a peptide; and
R
2
is hydrogen or lower C
1
-C
5
branched or straight alkyl,
or the salt or ester thereof, wherein
the stereochemistry about the carbon-carbon double bond is trans.
The invention further relates to a method for inducing an analgesic effect in a subject, comprising administering to the subject an effective amount of the compound having the structure I or II:
wherein,
R
1
is C
1
-C
10
branched or straight chain alkyl, aryl, an amino acid, or a peptide, and
R
2
is hydrogen or lower C
1
-C
5
branched or straight alkyl,
or the salt or ester thereof, wherein
the stereochemistry about the carbon-carbon double bond is trans.
The invention further provides a compound for reducing inflammation and/or inducing an analgesic effect having the structure II:
wherein, R
1
is an N-acyl amino acid or peptide,
or the salt or ester thereof.
Additional advantages of the invention will be set forth in part in the description which follows, and in part will be obvious from the description, or may be learned by practice of the invention. The advantages of the invention will be realized and attained by means of the elements and combinations particularly pointed out in the appended claims. It is to be understood that both the foregoing general description and the following detailed description are exemplary and explanatory only and are not restrictive of the invention, as claimed.


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